EP3615025A4 - Nrf and hif activators/hdac inhibitors and therapeutic methods using the same - Google Patents

Nrf and hif activators/hdac inhibitors and therapeutic methods using the same Download PDF

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Publication number
EP3615025A4
EP3615025A4 EP18790569.0A EP18790569A EP3615025A4 EP 3615025 A4 EP3615025 A4 EP 3615025A4 EP 18790569 A EP18790569 A EP 18790569A EP 3615025 A4 EP3615025 A4 EP 3615025A4
Authority
EP
European Patent Office
Prior art keywords
nrf
same
therapeutic methods
hdac inhibitors
hif activators
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP18790569.0A
Other languages
German (de)
French (fr)
Other versions
EP3615025A1 (en
Inventor
Irina GAISINA
Alan Kozikowski
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Illinois
Original Assignee
University of Illinois
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by University of Illinois filed Critical University of Illinois
Publication of EP3615025A1 publication Critical patent/EP3615025A1/en
Publication of EP3615025A4 publication Critical patent/EP3615025A4/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0446—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0453—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
EP18790569.0A 2017-04-26 2018-04-25 Nrf and hif activators/hdac inhibitors and therapeutic methods using the same Pending EP3615025A4 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762490101P 2017-04-26 2017-04-26
PCT/US2018/029258 WO2018200608A1 (en) 2017-04-26 2018-04-25 Nrf and hif activators/hdac inhibitors and therapeutic methods using the same

Publications (2)

Publication Number Publication Date
EP3615025A1 EP3615025A1 (en) 2020-03-04
EP3615025A4 true EP3615025A4 (en) 2020-11-25

Family

ID=63918693

Family Applications (1)

Application Number Title Priority Date Filing Date
EP18790569.0A Pending EP3615025A4 (en) 2017-04-26 2018-04-25 Nrf and hif activators/hdac inhibitors and therapeutic methods using the same

Country Status (9)

Country Link
US (1) US10934255B2 (en)
EP (1) EP3615025A4 (en)
JP (1) JP7396646B2 (en)
CN (1) CN110730660A (en)
AU (1) AU2018258338B2 (en)
CA (1) CA3056448A1 (en)
IL (1) IL269124B2 (en)
MX (1) MX2019012674A (en)
WO (1) WO2018200608A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102236356B1 (en) 2017-11-24 2021-04-05 주식회사 종근당 Compositions for Preventing or Treating Lupus
CN109574936B (en) * 2018-11-23 2022-02-22 沈阳药科大学 Hydroxamic acid compound with HDAC6 inhibitory activity and application thereof
US20220008414A1 (en) * 2018-11-23 2022-01-13 Chong Kun Dang Pharmaceutical Corp. Pharmaceutical composition comprising histone deacetylase 6 inhibitors
WO2020167969A1 (en) * 2019-02-15 2020-08-20 Triterpenoid Therapeutics, Inc. Methods and compositions for inhibiting the nlrp3 inflammasome and/or lon protease
MX2022004809A (en) * 2019-10-23 2022-05-16 Chong Kun Dang Pharmaceutical Corp Compositions for preventing or treating chronic obstructive pulmonary diseases (copd).
CN113527206B (en) 2020-04-17 2022-12-30 上海中泽医药科技有限公司 Benzoazaheterocycle compound, preparation method and application thereof
WO2021226261A1 (en) 2020-05-06 2021-11-11 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
CN112843038B (en) * 2021-03-30 2022-05-20 徐州医科大学 Application of medicine in preparation of medicine for treating diffuse large B cell lymphoma
WO2023192424A1 (en) * 2022-03-30 2023-10-05 The Regents Of The University Of California Volatile hd ac inhibitors for therapeutic and plant applications cross-reference to related application

Citations (4)

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Publication number Priority date Publication date Assignee Title
WO2007028638A1 (en) * 2005-09-09 2007-03-15 Euro-Celtique S.A. Fused and spirocycle compounds and the use thereof
WO2011011186A2 (en) * 2009-07-22 2011-01-27 The Board Of Trustees Of The University Of Illinois Hdac inhibitors and therapeutic methods using the same
WO2013062344A1 (en) * 2011-10-28 2013-05-02 Chong Kun Dang Pharmaceutical Corp. Hydroxamate derivatives for hdac inhibitor, and the pharmaceutical composition comprising thereof
WO2014181137A1 (en) * 2013-05-10 2014-11-13 Karus Therapeutics Ltd Novel histone deacetylase inhibitors

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US7528165B2 (en) * 2001-12-13 2009-05-05 National Health Research Institutes Indole compounds
US7408079B2 (en) 2002-01-10 2008-08-05 The Johns Hopkins University Imaging agents and methods of imaging NAALADase or PSMA
US20060183902A1 (en) 2005-02-15 2006-08-17 Baxter Ellen W Dihydroindolyl methanones as alpha 1a/1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms
UA95788C2 (en) 2005-12-15 2011-09-12 Ф. Хоффманн-Ля Рош Аг Fused pyrrole derivatives
JP2009525955A (en) * 2006-01-13 2009-07-16 タケダ サン ディエゴ インコーポレイテッド Histone deacetylase inhibitor
AU2007282080B2 (en) 2006-08-03 2013-06-27 Georgetown University Isoform-selective HDAC inhibitors
SI2343286T1 (en) 2006-10-28 2015-05-29 Methylgene Inc. Dibenzo(b,f)(1,4)oxazepine derivatives as inhibitors of histone deacetylase
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WO2017053360A1 (en) 2015-09-22 2017-03-30 The Board Of Trustees Of The University Of Illinois Bicyclic and tricyclic cap bearing mercaptoacetamide derivatives as histone deacetylase inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007028638A1 (en) * 2005-09-09 2007-03-15 Euro-Celtique S.A. Fused and spirocycle compounds and the use thereof
WO2011011186A2 (en) * 2009-07-22 2011-01-27 The Board Of Trustees Of The University Of Illinois Hdac inhibitors and therapeutic methods using the same
WO2013062344A1 (en) * 2011-10-28 2013-05-02 Chong Kun Dang Pharmaceutical Corp. Hydroxamate derivatives for hdac inhibitor, and the pharmaceutical composition comprising thereof
WO2014181137A1 (en) * 2013-05-10 2014-11-13 Karus Therapeutics Ltd Novel histone deacetylase inhibitors

Non-Patent Citations (2)

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Title
See also references of WO2018200608A1 *
TRAN-THI-LAN HUONG ET AL: "Novel N -hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity", BIOORGANIC CHEMISTRY., vol. 71, 1 April 2017 (2017-04-01), US, pages 160 - 169, XP055416602, ISSN: 0045-2068, DOI: 10.1016/j.bioorg.2017.02.002 *

Also Published As

Publication number Publication date
JP2020517688A (en) 2020-06-18
AU2018258338B2 (en) 2022-07-14
EP3615025A1 (en) 2020-03-04
IL269124A (en) 2019-11-28
CA3056448A1 (en) 2018-11-01
IL269124B1 (en) 2023-01-01
US20200039933A1 (en) 2020-02-06
MX2019012674A (en) 2020-02-05
CN110730660A (en) 2020-01-24
IL269124B2 (en) 2023-05-01
US10934255B2 (en) 2021-03-02
WO2018200608A1 (en) 2018-11-01
AU2018258338A1 (en) 2019-11-14
JP7396646B2 (en) 2023-12-12

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